DK3828173T3 - Substituerede pyrazoler som humant plasma-kallikreininhibitorer - Google Patents

Substituerede pyrazoler som humant plasma-kallikreininhibitorer Download PDF

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Publication number
DK3828173T3
DK3828173T3 DK20191747.3T DK20191747T DK3828173T3 DK 3828173 T3 DK3828173 T3 DK 3828173T3 DK 20191747 T DK20191747 T DK 20191747T DK 3828173 T3 DK3828173 T3 DK 3828173T3
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Prior art keywords
human plasma
plasma kallikrein
substituted pyrazoles
kallikrein inhibitors
inhibitors
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DK20191747.3T
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Danish (da)
English (en)
Inventor
Pravin L Kotian
Yarlagadda S Babu
Minwan Wu
Venkat R Chintareddy
Satish V Kumar
Weihe Zhang
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Biocryst Pharm Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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    • A61P7/10—Antioedematous agents; Diuretics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
DK20191747.3T 2014-03-07 2015-03-09 Substituerede pyrazoler som humant plasma-kallikreininhibitorer DK3828173T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461949808P 2014-03-07 2014-03-07
US201461981515P 2014-04-18 2014-04-18
EP15759254.4A EP3113772B8 (en) 2014-03-07 2015-03-09 Trifluoromethyl substituted pyrazoles as human plasma kallikrein inhibitors

Publications (1)

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DK3828173T3 true DK3828173T3 (da) 2022-11-07

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Application Number Title Priority Date Filing Date
DK15759254.4T DK3113772T3 (da) 2014-03-07 2015-03-09 Trifluormethylsubstituerede pyrazoler som inhibitorer af kallikrein fra humant plasma
DK20191747.3T DK3828173T3 (da) 2014-03-07 2015-03-09 Substituerede pyrazoler som humant plasma-kallikreininhibitorer

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DK15759254.4T DK3113772T3 (da) 2014-03-07 2015-03-09 Trifluormethylsubstituerede pyrazoler som inhibitorer af kallikrein fra humant plasma

Country Status (33)

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US (14) US10125102B2 (OSRAM)
EP (4) EP4663636A2 (OSRAM)
JP (4) JP6574435B2 (OSRAM)
KR (2) KR102510427B1 (OSRAM)
CN (2) CN106257976B (OSRAM)
AU (3) AU2015226855C1 (OSRAM)
BR (1) BR112016020199A8 (OSRAM)
CA (2) CA3164693A1 (OSRAM)
CY (2) CY1123810T1 (OSRAM)
DK (2) DK3113772T3 (OSRAM)
EA (1) EA036251B1 (OSRAM)
ES (3) ES2836373T3 (OSRAM)
FR (1) FR21C1048I2 (OSRAM)
HR (2) HRP20201916T1 (OSRAM)
HU (3) HUE052668T2 (OSRAM)
IL (2) IL280785B2 (OSRAM)
LT (3) LT3828173T (OSRAM)
LU (1) LUC00233I2 (OSRAM)
MA (1) MA53399B1 (OSRAM)
MX (2) MX2020013059A (OSRAM)
MY (1) MY199131A (OSRAM)
NL (1) NL301142I2 (OSRAM)
NO (1) NO2022046I1 (OSRAM)
NZ (2) NZ724250A (OSRAM)
PH (1) PH12016501750B1 (OSRAM)
PL (2) PL3828173T3 (OSRAM)
PT (2) PT3828173T (OSRAM)
RS (2) RS61159B1 (OSRAM)
SG (2) SG10202001795XA (OSRAM)
SI (1) SI3113772T1 (OSRAM)
SM (2) SMT202100031T1 (OSRAM)
WO (1) WO2015134998A1 (OSRAM)
ZA (1) ZA201606320B (OSRAM)

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TWI636047B (zh) 2013-08-14 2018-09-21 英商卡爾維斯塔製藥有限公司 雜環衍生物
GB2517908A (en) 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors
SG10201908467RA (en) 2014-01-31 2019-10-30 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2' groups as factor xia inhibitors
NO2760821T3 (OSRAM) 2014-01-31 2018-03-10
KR102510427B1 (ko) 2014-03-07 2023-03-14 바이오크리스트파마슈티컬즈,인코포레이티드 인간 혈장 칼리크레인 저해제
EP3189047B1 (en) 2014-09-04 2018-12-26 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
HRP20220059T1 (hr) 2015-10-01 2022-04-15 Biocryst Pharmaceuticals, Inc. Inhibitori kalikreina humane plazme
SMT202000382T1 (it) 2016-05-31 2020-09-10 Kalvista Pharmaceuticals Ltd Derivati di pirazolo come inibitori di callicreina plasmatica
GB201609603D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide
GB201609607D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts
PL3716952T3 (pl) 2017-11-29 2022-05-02 Kalvista Pharmaceuticals Limited Postacie dawkowania zawierające inhibitor kalikreiny osoczowej
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
GB201721515D0 (en) * 2017-12-21 2018-02-07 Kalvista Pharmaceuticals Ltd Dosage forms comprising a plasma kallikrein inhibtor
JP7538113B2 (ja) 2018-08-20 2024-08-21 アキリオン ファーマシューティカルズ，インコーポレーテッド 補体ｄ因子の医学的障害の治療のための医薬化合物
WO2020051532A2 (en) 2018-09-06 2020-03-12 Achillion Pharmaceuticals, Inc. Macrocyclic compounds for the treatment of medical disorders
AR116951A1 (es) * 2018-11-02 2021-06-30 Biocryst Pharm Inc Sales cristalinas de un inhibidor de calicreína plasmática
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AU2020273154A1 (en) * 2019-04-08 2021-12-02 Biocryst Pharmaceuticals, Inc. Plasma kallikrein inhibitors and methods of use thereof in ocular disorders
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TW202144331A (zh) * 2020-02-13 2021-12-01 德商百靈佳殷格翰國際股份有限公司 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物
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